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ES2140181T3 - ANDROSTENONAS. - Google Patents

ANDROSTENONAS.

Info

Publication number
ES2140181T3
ES2140181T3 ES97200658T ES97200658T ES2140181T3 ES 2140181 T3 ES2140181 T3 ES 2140181T3 ES 97200658 T ES97200658 T ES 97200658T ES 97200658 T ES97200658 T ES 97200658T ES 2140181 T3 ES2140181 T3 ES 2140181T3
Authority
ES
Spain
Prior art keywords
sup
hydrogen
carbon
halogen
atoms
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Lifetime
Application number
ES97200658T
Other languages
Spanish (es)
Inventor
Kenneth William Batchelor
Stephen Vernon Frye
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
SmithKline Beecham Corp
Original Assignee
Glaxo Wellcome Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Glaxo Wellcome Inc filed Critical Glaxo Wellcome Inc
Application granted granted Critical
Publication of ES2140181T3 publication Critical patent/ES2140181T3/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J3/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
    • C07J3/005—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom the carbon atom being part of a carboxylic function
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26—Androgens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/70—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/82—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0066—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by a carbon atom forming part of an amide group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • C07J73/001—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom
    • C07J73/005—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom by nitrogen as hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
    • C07C2603/14—Benz[f]indenes; Hydrogenated benz[f]indenes

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Transition And Organic Metals Composition Catalysts For Addition Polymerization (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)

Abstract

LA INVENCION DESCRIBE UN COMPUESTO DE FORMULA (I), DONDE LOS CARBONOS 1 Y 2, ESTAN UNIDOS POR UN ENLACE SIMPLE O DOBLE; R{SUP,1} ES HIDROGENO O METILO; R{SUP,2} ES HIDROGENO O METILO; R{SUP,3} ES (A) DONDE R{SUP,4} Y R{SUP,5} SON, INDEPENDIENTEMENTE, HIDROGENO, ALQUILO LINEAL O RAMIFICADO DE 1 A 6 ATOMOS DE CARBONO, ALCOXI LINEAL O RAMIFICADO DE 1 A 6 ATOMOS DE CARBONO, TRIFLUOROMETILO, CIANO, HALOGENO, FENILO (OPCIONALMENTE SUSTITUIDO CON UNO O MAS HALOGENOS), O, CUANDO R{SUP,4} Y R{SUP,5} ESTAN EN CARBONOS ADYACENTES, FORMAN CONJUNTAMENTE UN ANILLO DE 5, 6 O 7 MIEMBROS, QUE CONTIENE OPCIONALMENTE UNO O MAS ATOMOS DE OXIGENO O AZUFRE; W Y Z SON GRUPOS METILENO QUE, TOMADOS JUNTO CON EL CARBONO AL QUE ESTAN UNIDOS, FORMAN UN SISTEMA CICLICO SATURADO DE 3 A 12 MIEMBROS, OPCIONALMENTE: 1) SUSTITUIDO INDEPENDIENTEMENTE CON UNO O MAS GRUPOS ALQUILO INFERIORES, 2) QUE CONTIENE UN ATOMO DE OXIGENO O AZUFRE, 3) DOS DE LOS GRUPOS METILENO CITADOS, DE DICHO ANILLO DE 3 A 12 ESTAN UNIDOS A UN GRUPO ALQUILENO (C{SUB,1-6} PARA FORMAR UN SISTEMA BICICLICO; X ES HIDROGENO O HALOGENO; O UN SOLVATO FARMACEUTICAMENTE ACEPTABLE DEL MISMO.THE INVENTION DESCRIBES A COMPOUND OF FORMULA (I), WHERE CARBONS 1 AND 2 ARE UNITED BY A SIMPLE OR DOUBLE LINK; R {SUP, 1} IS HYDROGEN OR METHYL; R {SUP, 2} IS HYDROGEN OR METHYL; R {SUP, 3} IS (A) WHERE R {SUP, 4} AND R {SUP, 5} ARE, INDEPENDENTLY, HYDROGEN, LINEAR OR BRANCHED ALKYL OF 1 TO 6 CARBON ATOMS, LINEAR ALCOXY OR BRANCHED OF 1 TO 6 ATOMS CARBON, TRIFLUOROMETHYL, CYAN, HALOGEN, PHENYL (OPTIONALLY REPLACED WITH ONE OR MORE HALOGEN), OR, WHEN R {SUP, 4} AND R {SUP, 5} ARE IN ADJACENT CARBON, TOGETHER FORM A RING OF 5, 6 OR 7 MEMBERS, WHICH OPTIONALLY CONTAINS ONE OR MORE ATOMS OF OXYGEN OR SULFUR; WYZ ARE METHYLENE GROUPS WHICH, TAKEN TOGETHER WITH THE CARBON TO WHICH THEY ARE UNITED, FORM A SATURATED CYCLE SYSTEM OF 3 TO 12 MEMBERS, OPTIONALLY: 1) INDEPENDENTLY SUBSTITUTED WITH ONE OR MORE LOWER ALKYL GROUPS, 2) WHICH CONTAINS AN OENYX SULFUR, 3) TWO OF THE MENTIONED METHYLENE GROUPS, FROM SUCH A RING OF 3 TO 12 ARE JOINED TO AN ALKYLENE GROUP (C {SUB, 1-6} TO FORM A BICYCLE SYSTEM; X IS HYDROGEN OR HALOGEN; OR A PHARMACEUTICALLY ACCEPTABLE SOLVATE OF THE SAME.

ES97200658T 1993-09-17 1994-09-16 ANDROSTENONAS. Expired - Lifetime ES2140181T3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US12328093A 1993-09-17 1993-09-17
US13651593A 1993-10-12 1993-10-12

Publications (1)

Publication Number Publication Date
ES2140181T3 true ES2140181T3 (en) 2000-02-16

Family

ID=26821398

Family Applications (2)

Application Number Title Priority Date Filing Date
ES94928605T Expired - Lifetime ES2110260T3 (en) 1993-09-17 1994-09-16 ANDROSTENONAS.
ES97200658T Expired - Lifetime ES2140181T3 (en) 1993-09-17 1994-09-16 ANDROSTENONAS.

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ES94928605T Expired - Lifetime ES2110260T3 (en) 1993-09-17 1994-09-16 ANDROSTENONAS.

Country Status (19)

Country Link
US (1) US5977126A (en)
EP (2) EP0783001B1 (en)
CN (1) CN1041939C (en)
AT (2) ATE161268T1 (en)
AU (1) AU685167B2 (en)
CA (3) CA2449679C (en)
DE (2) DE69421726T2 (en)
DK (2) DK0783001T3 (en)
ES (2) ES2110260T3 (en)
FI (1) FI961232A0 (en)
GR (2) GR3025717T3 (en)
HU (1) HUT74445A (en)
IL (1) IL110979A (en)
IS (1) IS1726B (en)
NO (1) NO306510B1 (en)
NZ (1) NZ274059A (en)
RU (1) RU2144037C1 (en)
TW (1) TW408127B (en)
WO (1) WO1995007926A1 (en)

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TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
US6001844A (en) * 1995-09-15 1999-12-14 Merck & Co., Inc. 4-Azasteroids for treatment of hyperandrogenic conditions
US5935968A (en) 1997-03-17 1999-08-10 Merck & Co., Inc. Methods for treating polycystic ovary syndrome
GB9717444D0 (en) * 1997-08-19 1997-10-22 Glaxo Group Ltd Pharmaceutical composition
GB9717428D0 (en) * 1997-08-19 1997-10-22 Glaxo Group Ltd Pharmaceutical composition
EP1832598A3 (en) 1999-09-30 2008-01-02 Hollis-Eden Pharmaceuticals Inc. Therapeutic treatment of androgen receptor driven conditions
GB0026876D0 (en) * 2000-11-03 2000-12-20 Glaxo Group Ltd Process
AU1076802A (en) * 2000-11-03 2002-05-15 Matrix Therapeutics Ltd Selective glucocorticoid receptor agonists
US6645974B2 (en) 2001-07-31 2003-11-11 Merck & Co., Inc. Androgen receptor modulators and methods for use thereof
AU2002331916B2 (en) * 2001-10-03 2008-07-24 Merck Sharp & Dohme Corp. Androstane 17-beta-carboxamides as androgen receptor modulators
US7186838B2 (en) * 2002-03-13 2007-03-06 Merck & Co., Inc. Fluorinated 4-azasteroid derivatives as androgen receptor modulators
WO2003092588A2 (en) * 2002-04-30 2003-11-13 Merck & Co., Inc. 4-azasteroid derivatives as androgen receptor modulators
CU23256A1 (en) * 2003-03-20 2008-01-24 Dalmer Lab Sa EXTRACT OBTAINED FROM ROYSTONEA REGIA FRUITS USED AGAINST PROSTATE HYPERPLASIA AND PROSTATITIS
WO2005105091A1 (en) * 2004-04-28 2005-11-10 Merck & Co., Inc. Fluorinated 4-azasteroids as androgen receptor modulators
HU230730B1 (en) 2011-06-30 2017-12-28 Richter Gedeon Nyrt Process for the preparation of (5alpha,17beta)-n-[2,5-bis-(trifluoromethyl)-phenyl]-3-oxo-4-aza-5-androst-1-en-17-carboxylic amide
CN103554213A (en) * 2012-01-05 2014-02-05 中国药科大学 4-oxa-androstane-3-ketone-17beta-amides derivatives, as well as preparation method and medical applications thereof
CN102532236B (en) * 2012-01-05 2014-04-16 中国药科大学 Steroidal 5α-reductase inhibitor, its preparation method and its medical use
CN103570796A (en) * 2012-07-24 2014-02-12 重庆医药工业研究院有限责任公司 Preparation method of dutasteride type-I crystal

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AU527030B2 (en) * 1978-04-13 1983-02-10 Merck & Co., Inc. 4-aza-17-substituted-5a-androstan-3-ones
US4377584A (en) * 1978-04-13 1983-03-22 Merck & Co., Inc. 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors
US4760071A (en) * 1984-02-27 1988-07-26 Merck & Co., Inc. 17β-N-monosubstituted carbamoyl-4-aza-5α-androst-1-en-3-ones which are active as testosterone 5α-reductase inhibitors
US5049562A (en) * 1984-02-27 1991-09-17 Merck & Co., Inc. 17β-acyl-4-aza-5α-androst-1-ene-3-ones as 5α-reductase inhibitors
US4845104A (en) * 1986-11-20 1989-07-04 Merck & Co., Inc. Oxidized analogs of 17β-N-monosubstituted-carbamoyl-4-aza-5-α-androstan-3-ones
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Also Published As

Publication number Publication date
ATE186733T1 (en) 1999-12-15
FI961232A7 (en) 1996-03-15
CA2449679C (en) 2007-10-23
CA2478971C (en) 2007-10-23
GR3025717T3 (en) 1998-03-31
CN1041939C (en) 1999-02-03
ES2110260T3 (en) 1998-02-01
GR3032198T3 (en) 2000-04-27
DK0719277T3 (en) 1998-08-24
ATE161268T1 (en) 1998-01-15
CA2449679A1 (en) 1995-03-23
DE69421726T2 (en) 2000-06-29
CA2478971A1 (en) 1995-03-23
RU2144037C1 (en) 2000-01-10
AU685167B2 (en) 1998-01-15
DE69421726D1 (en) 1999-12-23
FI961232L (en) 1996-03-15
NO961085L (en) 1996-04-22
EP0783001A1 (en) 1997-07-09
IS4206A (en) 1995-03-18
NO961085D0 (en) 1996-03-15
FI961232A0 (en) 1996-03-15
IL110979A (en) 1999-08-17
DE69407422D1 (en) 1998-01-29
CA2171329C (en) 2004-11-23
IL110979A0 (en) 1994-11-28
EP0719277B1 (en) 1997-12-17
NZ274059A (en) 1997-12-19
WO1995007926A1 (en) 1995-03-23
EP0783001B1 (en) 1999-11-17
HUT74445A (en) 1996-12-30
CA2171329A1 (en) 1995-03-23
IS1726B (en) 1999-09-06
AU7798094A (en) 1995-04-03
DE69407422T2 (en) 1998-04-09
HU9600643D0 (en) 1996-05-28
CN1134155A (en) 1996-10-23
NO306510B1 (en) 1999-11-15
EP0719277A1 (en) 1996-07-03
TW408127B (en) 2000-10-11
US5977126A (en) 1999-11-02
DK0783001T3 (en) 2000-04-10

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